Design and Synthesis of Oxime Ethers of β-Oxo-γ-phenylbutanoic Acids as PPAR α and -γ Dual Agonists

Oxime ethers of β-oxo-γ-phenylbutanoic acids were prepared to develop more effective PPAR α and γ dual agonists. Among them, compound 11k exhibited potent in vitro activities with EC50 of 2.5 nM and 3.3 nM in PPAR α and γ, respectively. It showed better glucose lowering effects than rosiglitazone 1...

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Published in:Bulletin of the Korean Chemical Society 2012, 33(6), , pp.1979-1982
Main Authors: Han, Hee-Oon, Koh, Jong-Sung, Kim, Seung-Hae, Park, Ok-Ku, Kim, Kyoung-Hee, Jeon, Sang-Kweon, Hur, Gwong-Cheung, Yim, Hyeon-Joo, Kim, Geun-Tae
Format: Article
Language:English
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화학
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Summary:Oxime ethers of β-oxo-γ-phenylbutanoic acids were prepared to develop more effective PPAR α and γ dual agonists. Among them, compound 11k exhibited potent in vitro activities with EC50 of 2.5 nM and 3.3 nM in PPAR α and γ, respectively. It showed better glucose lowering effects than rosiglitazone 1 and improved the lipid profile like plasma triglyceride in db/db mice model. KCI Citation Count: 3
ISSN:0253-2964
1229-5949
DOI:10.5012/bkcs.2012.33.6.1979